Receptor-Ligand Kinetics

The receptor-ligand kinetics is typically described by the chemical reaction:

\[R + L \rightleftharpoons RL\]

where \(R\) is the receptor, \(L\) is the ligand, and \(RL\) is the ligand-receptor complex. The reaction is characterized by the on-rate constant \(k_{on}\) and the off-rate constant \(k_{off}\).

Association and Dissociation constants

At equilibrium, the rate of association is equal to the rate of dissociation:

\[k_{on}[R][L] = k_{off}[RL]\]

The equilibrium association constant is defined as:

\[K_a = \frac{k_{on}}{k_{off}}\]

and the dissociation constant \(K_d\) is its inverse. These constants are usually measured experimentally to describe the kinetics of the receptor-ligand interaction. A high \(K_a\) indicates a strong binding, while a high \(K_d\) indicates a weak binding (the inverse is true for \(K_d\)).

Experimental methods

The experimental methods used to investigate the kinetics of receptor-ligand interactions includes: ligand binding assays, crystallographic analysis, all atom MD simulations.

References

  1. Wikipedia
  2. Yao, Yongneng, et al. “Molecular mechanism of ligand recognition by NR3 subtype glutamate receptors.” The EMBO journal 27.15 (2008): 2158-2170.